Frontier Laboratories for Value Creation, Sapporo Holdings Ltd., 10 Okatome, Yaizu, Shizuoka 425-0013, Japan.
Department of Pharmacy, The University of Tokyo Hospital, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-8655, Japan.
Nutrients. 2020 May 29;12(6):1601. doi: 10.3390/nu12061601.
The beneficial effects of fatty acids (FAs) on human health have attracted widespread interest. However, little is known about the impact of FAs on the handling of urate, the end-product of human purine metabolism, in the body. Increased serum urate levels occur in hyperuricemia, a disease that can lead to gout. In humans, urate filtered by the glomerulus of the kidney is majorly re-absorbed from primary urine into the blood via the urate transporter 1 (URAT1)-mediated pathway. URAT1 inhibition, thus, contributes to decreasing serum urate concentration by increasing net renal urate excretion. Here, we investigated the URAT1-inhibitory effects of 25 FAs that are commonly contained in foods or produced in the body. For this purpose, we conducted an in vitro transport assay using cells transiently expressing URAT1. Our results showed that unsaturated FAs, especially long-chain unsaturated FAs, inhibited URAT1 more strongly than saturated FAs. Among the tested unsaturated FAs, eicosapentaenoic acid, α-linolenic acid, and docosahexaenoic acid exhibited substantial URAT1-inhibitory activities, with half maximal inhibitory concentration values of 6.0, 14.2, and 15.2 μM, respectively. Although further studies are required to investigate whether the ω-3 polyunsaturated FAs can be employed as uricosuric agents, our findings further confirm FAs as nutritionally important substances influencing human health.
脂肪酸（FAs）对人类健康的有益影响引起了广泛关注。然而，人们对 FAs 如何影响人体中尿酸（嘌呤代谢的终产物）的处理知之甚少。高尿酸血症会导致血清尿酸水平升高，进而引发痛风。在人类中，肾小球滤过的尿酸主要通过尿酸转运蛋白 1（URAT1）介导的途径从初级尿液中被重吸收回血液。因此，URAT1 抑制作用可通过增加净肾尿酸排泄来降低血清尿酸浓度。在这里，我们研究了 25 种常见于食物或体内产生的脂肪酸对 URAT1 的抑制作用。为此，我们使用瞬时表达 URAT1 的细胞进行了体外转运实验。结果表明，不饱和脂肪酸，特别是长链不饱和脂肪酸，对 URAT1 的抑制作用强于饱和脂肪酸。在测试的不饱和脂肪酸中，二十碳五烯酸、α-亚麻酸和二十二碳六烯酸对 URAT1 具有显著的抑制活性，其半最大抑制浓度值分别为 6.0、14.2 和 15.2 μM。尽管还需要进一步研究以探讨 ω-3 多不饱和脂肪酸是否可用作尿酸排泄剂，但我们的发现进一步证实了脂肪酸作为影响人类健康的重要营养物质。
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